Agmatine blocked voltage-gated calcium channel in cultured rat hippocampal neurons.

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Weng XC, Gai XD, Zheng JQ, Li J

Agmatine blocked voltage-gated calcium channel in cultured rat hippocampal neurons.

Acta Pharmacol Sin. 2003 Aug;24(8):746-50.

PubMed ID

12904272 [ View in PubMed

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Abstract

AIM: To investigate the mechanism of agmatine by observing the effect of agmatine on the voltage-gated channels in rat hippocampal neurons. METHODS: The whole-cell patch recording technique was performed to record the voltage-gated potassium, sodium, and calcium currents in cultured rat hippocampus. Agmatine was applied directly to the single neuron using a pressure injector with microtubules. RESULTS: Agmatine (500 micromol/L) had no significant effect on the voltage-gated potassium and sodium channels. Agmatine reversibly blocked the voltage-gated calcium channel and the blockade was enhanced with the increasing concentration of agmatine. The inhibitory rates were 21%+/-4%, 35%+/-6%, 49%+/-6%, 67%+/-4%, 69%+/-6%, 86%+/-8%, and 87%+/- 9%, at the concentration of 0.1, 0.5, 1.0, 5.0, 10.0, 50.0, and 100 micromol/L, respectively. IC50 was (1.2+/-0.4) micromol/L. Two-way ANOVA revealed that change of membrane potential displayed a significant interaction with the blockade by agmatine. CONCLUSION: Agmatine reversibly blocked the voltage-gated calcium channel in rat hippocampal neurons in a concentration- and voltage-dependent way. Agmatine might perform its physiological and pharmacological effects partially by blocking the calcium channel.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Agmatine	Voltage-dependent N-type calcium channel subunit alpha-1B	Protein	Humans	Yes	Antagonist	Details